Park Pyo-Jam, Ahn Chang-Bum, Jeon You-Jin, Je Jae-Young
Department of Biotechnology, Kunkuk University, Chungju 380-701, Republic of Korea.
Bioorg Med Chem Lett. 2008 Apr 1;18(7):2471-4. doi: 10.1016/j.bmcl.2008.02.041. Epub 2008 Feb 19.
Six kinds of chitooligosaccharides (COSs) with different molecular weight (MW) and degree of deacetylation (DD) were prepared using ultrafiltration membrane reactor, and their renin inhibition modes were evaluated. All the COSs showed the renin-inhibitory activities with dose-dependent manner, and 90-COSs had the potent renin-inhibitory activity than that of 50-COSs. Among them, 90-MMWCOS (1000-5000Da) exhibits the highest activity with IC(50) value of 0.51mg/mL and acts as competitive inhibitor with K(i) value of 0.28mg/mL by Lineweaver-Burk and Dixon plots. These results indicated that DD value and MW of COSs are important factors affecting renin-inhibitory activity.
使用超滤膜反应器制备了六种不同分子量(MW)和脱乙酰度(DD)的壳寡糖(COSs),并对它们的肾素抑制模式进行了评估。所有的COSs均呈现出剂量依赖性的肾素抑制活性,且90-COSs比50-COSs具有更强的肾素抑制活性。其中,90-MMWCOS(1000-5000Da)表现出最高活性,IC(50)值为0.51mg/mL,通过Lineweaver-Burk和Dixon作图法表明其作为竞争性抑制剂,K(i)值为0.28mg/mL。这些结果表明,COSs的DD值和MW是影响肾素抑制活性的重要因素。